Raloxifene is indicated for the treatment of osteoporosis and breast cancer in postmenopausal women. It is commercially available as immediate release tablets (Evista®) in the U.S. The development of raloxifene composition has been hindered, due to low water solubility which can adversely affect the bioavailability and manufacturing process. U.S. Pat. No. 6,458,811 discloses raloxifene having a mean particle size of less than 25 microns, which allows enhanced bioavailability and control during the manufacturing process. It further discloses granular compositions comprising raloxifene, which can be compressed into tablet dosage forms or can be filled into capsules.
Raloxifene is known to possess a bitter taste. Raloxifene is categorized as a drug that should be “handled as hazardous” by the National Institute for Occupational Safety and Health (U.S.). Further, the summary of product characteristic by the European Medicines Agency instructs to “not break or crush” Evista® tablets, as they may taste bad. Handling of uncoated granules and crushed tablets would also be hazardous for the compounding pharmacist.
Thus, there exists a need in the art to formulate a composition of raloxifene which provides for better patient compliance for patients that have difficulty in swallowing. However, masking the bitter taste as well as achieving the desired immediate release profile would be challenging for a drug with poor aqueous solubility.
Hence, the present inventors have now developed plurality of particulates of raloxifene, which can be administered by sprinkling multiparticulates on soft food and have a desired in-vitro release. The present invention would provide advantages for patients who have difficulty in swallowing the conventional solid oral composition. Further, the sprinkle composition of the present invention has high drug-loading, leading to a minimal total weight of the composition, which can be easily handled and taken by the patients.